For research use only. Not for therapeutic Use.
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells[1][2].
INDY (0.3-30 μM; 20 hours) mildly inhibits tau-phosphorylation at 3 μM, and nearly completely inhibits at 30 μM[1].
INDY effectively reverses the aberrant tau-phosphorylation and rescues the repressed NFAT (nuclear factor of activated T cell) signalling induced by Dyrk1A (dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A) overexpression[1].
ProINDY (2.5 μM) recoveres apparently normal development of the Xenopus embryo[1].
| Catalog Number | R031459 |
| CAS Number | 1169755-45-6 |
| Synonyms | (1Z)-1-(3-ethyl-5-hydroxy-1,3-benzothiazol-2-ylidene)propan-2-one |
| Molecular Formula | C12H13NO2S |
| Purity | ≥95% |
| InChI | InChI=1S/C12H13NO2S/c1-3-13-10-7-9(15)4-5-11(10)16-12(13)6-8(2)14/h4-7,15H,3H2,1-2H3/b12-6- |
| InChIKey | GCSZJMUFYOAHFY-SDQBBNPISA-N |
| SMILES | CCN1C2=C(C=CC(=C2)O)SC1=CC(=O)C |
| Reference | [1]. Ogawa Y, et al. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat Commun. 2010 Oct 5;1:86. [2]. Pozo N, et al. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastomagrowth. J Clin Invest. 2013 Jun;123(6):2475-87. |
